|Description||A high affinity pan-RAR antagonist (AGN194310, K(d) for binding to RARs = 2-5 nM) inhibited colony formation (by 50%) by all three lines at 16-34 nM, and led to a transient accumulation of flask-cultured cells in G1 followed by apoptosis. AGN194310 is 12-22 fold more potent than all-trans retinoic acid (ATRA) against cell lines and also more potent in inhibiting the growth of primary prostate carcinoma cells. The administration of all-trans retinoic acid to VAD mice resulted in a transient reduction in NF-kappaB activity and, conversely, a single dose of the RAR-pan-antagonist, AGN 194310, administered to control mice, led to a marked, transient induction of whole-body luminescence. Mice were treated with AGN194310, a synthetic retinoid that antagonises the physiological function of the three RAR isotypes (alpha, beta, gamma) but does not interact with RXRs. Analyses of the granulocytic lineage using Gr-1, c-Kit and CD11b antibodies, demonstrated that granulocyte numbers were strikingly increased across haemopoietic compartments in all AGN194310-treated mice. A significant increase in the frequency of progenitor cells containing granulocytes was observed in the bone marrow of mice following treatment with AGN194310.|
|Synonyms||AGN194310; AGN-194310; VTP194310; VTP 194310; VTP-194310|
UAB30 is a low-toxicity retinoid X receptor-selective agonist selective for the binding and activation of RXR’s over RAR' s. UAB30 is highly effective in the pr...
Bexarotene is a retinoid specifically selective for retinoid X receptors, used as an oral antineoplastic agent in the treatment of cutaneous T-cell lymphoma.
AM580 is a stable retinobenzoic derivative originally synthesized as a RARα agonist (EC50 values are 0.3, 8.6 and 13 nM for RARα, RARβ and RARγ respectively).
Fenretinide is an orally-active synthetic phenylretinamide analogue of retinol (vitamin A) with potential antineoplastic and chemopreventive activities. Fenreti...
CD1530 is a potent and selective retinoic acid receptor(RAR) agonist with Ki values of 150, 1500 and 2750 nM for RARγ, RARβ and RARα receptors respectively. It ...
Acitretin is a second generation retinoid used for psoriasis.
Adapalene is more active than indomethacin, betamethasone valerate, tretinoin, isotretinoin or etretinate in inhibiting lipoxygease activity, but it has little ...
TTNPB potently and selectively activates retinoic acid receptors (EC50s = 21, 4, and 2.4 nM for RARα, RARβ, and RARγ, respectively). And it does not act on reti...
Isotretinoin, also known as 13-cis retinoic acid and first marketed as Accutane by Hoffmann-La Roche, is an oral pharmaceutical drug primarily used to treat cys...
AGN 205728 is a potent and selective RARγ antagonist and has no inhibiton on RARα and RARβ.
Adapalene sodium salt
Adapalene sodium salt, a synthetic retinoid, is a Retinoic acid receptor agonist (RAR). It is a third-generation topical retinoid primarily used in the treatmen...
Palovarotene is a selective retinoic acid receptor gamma(RAR-γ) agonist for the treatment of emphysema. In small animal studies, palovarotene was claimed to rev...
HX-603 is a RXR agonist.
Acitretin sodium is a second-generation, systemic retinoid that has been used in the treatment of psoriasis. It can be considered one of the treatments of choic...
RX-195183 is an RARα agonist (Kd=3 nM) with potential antineoplastic activity, modulating the transcription of genes responsible for cell differentiation and pr...
Tazarotene could propel either early or late portions of the period leading to differentiation and G0 arrest and is interchangeable with an RARalpha-selective l...
Tamibarotene is a retinoic acid receptor α (RARα) agonist that induces differentiation and apoptosis of HL-60 cells in vitro. It exhibits antiproliferative effe...
NRX-204647 is a Retinoic acid receptor gamma-selective inverse agonist.
AGN 196996 is a potent and selective antagonist of RARα. It has been reported to selectively bind to RARs (retinoic acid receptors) for RARα, RARβ and RARγ. It...
A high affinity pan-RAR antagonist (AGN194310, K(d) for binding to RARs = 2-5 nM) inhibited colony formation (by 50%) by all three lines at 16-34 nM, and led to...